Research progress of ERK small molecule inhibitors
10.11665/j.issn.1000-5048.20200302
- VernacularTitle:小分子ERK抑制剂的研究进展
- Author:
Tingting LIANG
1
;
Wenjie WANG
;
Guangchao HE
;
Guangchao HE
;
Yungen XU
Author Information
1. 中国药科大学药物化学系
- Publication Type:Journal Article
- Keywords:
extracellular signal-regulated kinase (ERK);
ERK inhibitors;
antitumor;
drug resistance
- From:
Journal of China Pharmaceutical University
2020;51(3):260-269
- CountryChina
- Language:Chinese
-
Abstract:
Extracellular signal-regulated kinase (ERK) is a kind of serine/threonine protein kinase. As a key downstream protein in RAS-RAF-MEK-ERK signaling pathway, its abnormal activation plays an important role in the development of tumors. Selective ERK1/2 inhibitors can block ERK signaling pathway while overcoming drug resistance caused by upstream target mutation. In this paper, the components of MAPK signaling pathway, the structure and functions of ERK and the role of ERK signaling pathway in tumor development are summarized, and some representative ERK inhibitors in clinical or preclinical studies are emphasized.
